212779-48-1

Usage

Uses

Used in Pharmaceutical Industry:
Compound 52 is used as a research tool for studying the role of cyclin-dependent kinases in various cellular processes. Its ability to inhibit specific yeast cyclin-dependent kinases makes it a valuable compound for understanding the mechanisms of these enzymes and their potential as therapeutic targets.
Used in Cancer Research:
Compound 52 is used as a potential anticancer agent, as it inhibits the growth of S. cerevisiae, a model organism for studying cancer-related pathways. Its effectiveness in inhibiting the growth of cancer cells may provide insights into the development of new cancer therapies.
Used in Drug Development:
As an analog of purvalanol A, a potent inhibitor of mammalian cyclin-dependent kinases, Compound 52 can be used in the development of new drugs targeting these enzymes. Its cell permeability and specificity for certain cyclin-dependent kinases make it a promising candidate for further research and development in the pharmaceutical industry.

Upstream product

• 141-43-5 ethanolamine 
• 190654-78-5 (2-chloro-9-isopropyl-9H-purin-6-yl)(3-chlorophenyl)amine 
• 108-42-9 3-chloro-aniline 
• 5451-40-1 2,6 dichloropurine 
• 190654-76-3 2-chloro-6-(3-chlorophenylamino)-purine 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer

In the current study, we have designed and synthesized a series of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent kinase2 (CDK2) dual inhibitors by integrating purine-based pharmacophore into the recognition cap group of CS055. The representative compound 14d with excellent antiproliferative activities towards five solid cancer cells, showed potent inhibitory activities against HDAC1, HDAC2 and CDK2 with IC50 values of 70.7 nM, 23.1 nM and 0.80 μM, respectively. Besides, compound 14d could effectively block the cell cycle in the G2/M phase and induce apoptosis, which might be related to increasing intracellular ROS levels. Importantly, compound 14d exhibited desirable pharmacokinetic (PK) properties with the intraperitoneal bioavailability of 50.8percent in ICR mice, and potent in vivo antitumor activity in the HCT116 xenograft model. Therefore, compound 14d could be considered as a promising lead compound for the development of multitargeting anticancer agents.

Synthesis and biological properties of C-2, C-8, N-9 substituted 6-(3-chloroanilino)-purine derivatives as cyclin-dependent kinase inhibitors. Part II

In this study, C-2, C-8, N-9 substituted 6-(3-chloroanilino)purine derivatives were synthesized and their inhibitory effects on cyclin-dependent kinases (CDK2, 4) as well as their cytotoxicities were evaluated. The effects of substituents at the C-2, C-8, and N-9 positions of the substituted purine were investigated. Among the compounds tested, [6-(3-chloroanilino)-2-(2-hydroxymethyl-4-hydroxypyrrolidyl)- 9-isopropylpurine] (4h) was the most active inhibitor of CDK2 with IC50 of 0.3μM i.e. a two-fold increased inhibitory activity as compared to roscovitine. Results from structure-activity relationship studies should allow the design of more potent and selective CDK2 inhibitors, which may provide an effective therapy for cancer or other CDK-dependent diseases.